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rdf:type |
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lifeskim:mentions |
umls-concept:C0019643,
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0037083,
umls-concept:C0205246,
umls-concept:C0243072,
umls-concept:C0387337,
umls-concept:C1259731,
umls-concept:C1422386,
umls-concept:C1510438,
umls-concept:C1710082,
umls-concept:C2603343
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pubmed:issue |
6
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pubmed:dateCreated |
2009-3-20
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pubmed:abstractText |
The Wnt signaling pathway regulates cell growth and development in metazoans, and is therefore of interest for drug discovery. By screening a library of 5808 pre-fractionated marine extracts in a cell-based Wnt signaling assay, several signaling activators and inhibitors were observed. LCMS-based fractionation rapidly identified an active compound from Pseudoceratina purpurea as psammaplin A, a known HDAC inhibitor. Other HDAC inhibitors similarly activated signaling in this assay, indicating HDAC inhibitors will be identified through many cell-based reporter assays. In a large scale analysis of P. purpurea, three previously undescribed bromotyrosine based natural products were identified; the structure of one of these was confirmed by synthesis. Additionally, three other derivatives of psammaplin A were prepared: a mixed disulfide and two sulfinate esters. Finally, evidence to support a structural reassignment of psammaplin I from a sulfone to the isomeric sulfinate ester is presented.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-10200307,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-10667200,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-10757728,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-12199561,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-12737565,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-14640526,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-15035989,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-15095382,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-15620274,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-15686623,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-16146364,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-17070060,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-17433686,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-17884696,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-3276306,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-9501205,
http://linkedlifedata.com/resource/pubmed/commentcorrection/19022675-9599273
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1464-3391
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2189-98
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pubmed:dateRevised |
2010-9-23
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pubmed:meshHeading |
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pubmed:year |
2009
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pubmed:articleTitle |
Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives.
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pubmed:affiliation |
Department of Medicinal Chemistry, University of Utah, Salt Lake City, UT 84112, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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